Description
Cilostamide (68550-75-4) is a selective inhibitor of phosphodiesterase-3 (PDE3). Displays limited selectivity for PDE3A versus PDE3B (IC50 = 27 and 50 nM).1,2 Blocks PKB/Akt signaling pathway downstream via inhibition of Akt-activated PDE3B.3 Cilostamide reverses the effect of leptin on food intake and body weight.4
Biological Activity
Selective inhibitor of type III phosphodiesterase (PDE3). Displays moderate selectivity for PDE3A isozyme vs. PDE3B (IC 50 values are 0.027 and 0.050 μ M for PDE3A and PDE3B respectively). Inhibits ADP-induced platelet aggregation (IC 50 = 16.8 μ M); anti-thrombotic. Also available as part of the Phosphodiesterase Inhibitor Tocriset™ .
References
[1] H HIDAKA. Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation.[J]. Journal of Pharmacology and Experimental Therapeutics, 1979, 211 1: 26-30.
[2] S. CHRISTENSEN T T. Chapter 19. Isozyme-Selective Phosphodiesterase Inhibitors as Antiasthmatic Agents[J]. Annual Reports in Medicinal Chemistry, 1994, 29 1: 185-194. DOI:
10.1016/s0065-7743(08)60732-0[3] F AHMAD. Cyclic nucleotide phosphodiesterase 3B is a downstream target of protein kinase B and may be involved in regulation of effects of protein kinase B on thymidine incorporation in FDCP2 cells.[J]. Journal of immunology, 2000, 164 9: 4678-4688. DOI:
10.4049/jimmunol.164.9.4678[4] ALLAN Z. ZHAO. A phosphatidylinositol 3-kinase–phosphodiesterase 3B–cyclic AMP pathway in hypothalamic action of leptin on feeding[J]. Nature neuroscience, 2002, 5 8: 727-728. DOI:
10.1038/nn885
